CLOTRIMAZOLE TOPICAL SOLUTION USP, 1% - clotrimazole topical solution usp, 1% solution

United States - English - NLM (National Library of Medicine)

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Active ingredient:
Clotrimazole (UNII: G07GZ97H65) (Clotrimazole - UNII:G07GZ97H65)
Available from:
Tasman Pharma Inc.
Administration route:
TOPICAL
Prescription type:
PRESCRIPTION DRUG
Therapeutic indications:
Prescription clotrimazole topical solution product is indicated for the topical treatment of candidiasis due to Candida albicans and tinea versicolor due to Malassezia furfur . This formulation is also available as a nonprescription product which is indicated for the topical treatment of the following dermal infections: tinea pedis, tinea cruris, and tinea corporis due to Trichophyton rubrum, Trichophyton mentagrophytes , Epidermophyton fluoccosum , and Microsporum canis . Topical antifungal agents are contraindicated in those patients with a history of hypersensitivity to any of the components of the preparation.
Product summary:
Clotrimazole topical solution USP, 1% is supplied in 30 mL plastic bottles (NDC 72641-001-30); boxes of one. Store between 2° to 30°C (36° to 86°F).
Authorization status:
Abbreviated New Drug Application
Authorization number:
72641-001-30

CLOTRIMAZOLE TOPICAL SOLUTION USP, 1% - clotrimazole topical solution usp,

1% solution

Tasman Pharma Inc.

----------

Clotrimazole Topical Solution USP, 1%

FOR EXTERNAL USE ONLY.

NOT FOR OPHTHALMIC USE.

This product is also available without a prescription.

Rx Only

DESCRIPTION

Clotrimazole topical solution USP, 1% contains 10 mg clotrimazole USP, a synthetic antifungal agent

having the chemical name 1-(o-Chloro-α,α-diphenylbenzyl) imidazole with the following structural

formula:

MOLECULAR FORMULA C

H CIN

MOLECULAR WEIGHT 344.85

Clotrimazole is an odorless, white crystalline substance. It is practically insoluble in water, sparingly

soluble in ether and very soluble in polyethylene glycol 400, ethanol, and chloroform.

Each mL of clotrimazole topical solution USP, 1% contains 10 mg clotrimazole USP in a nonaqueous

vehicle of polyethylene glycol 400.

CLINICAL PHARMACOLOGY

Clotrimazole is a broad-spectrum antifungal agent that is used for the treatment of dermal infections

caused by various species of pathogenic dermatophytes, yeasts, and Malassezia furfur. The primary

action of clotrimazole is against dividing and growing organisms.

In vitro, clotrimazole exhibits fungistatic and fungicidal activity against isolates of Trichophyton rubrum,

Trichophyton mentagrophytes, Epidermophyton floccosum, Microsporum canis, and Candida species

including Candida albicans. In general, the in vitro activity of clotrimazole corresponds to that of

tolnaftate and griseofulvin against the mycelia of dermatophytes (Trichophyton, Microsporum, and

Epidermophyton), and to that of the polyenes (amphotericin B and nystatin) against budding fungi

(Candida). Using an in vivo (mouse) and an in vitro (mouse kidney homogenate) testing system,

clotrimazole and miconazole were equally effective in preventing the growth of the pseudomycelia and

mycelia of Candida albicans.

Strains of fungi having a natural resistance to clotrimazole are rare. Only a single isolate of Candida

guilliermondi has been reported to have primary resistance to clotrimazole.

No single-step or multiple-step resistance to clotrimazole has developed during successive passages

of Candida albicans and Trichophyton mentagrophytes. No appreciable change in sensitivity was detected

after successive passages of isolates of C. albicans, C. krusei, or C. pseudotropicalis in liquid or solid

media containing clotrimazole. Also, resistance could not be developed in chemically induced mutant

strains of polyene-resistant isolates of C. albicans.

Slight, reversible resistance was noted in three isolates of C. albicans tested by one investigator. There

is a single report that records the clinical emergence of a C. albicans strain with considerable resistance

to flucytosine and miconazole, and with cross-resistance to clotrimazole; the strain remained sensitive

to nystatin and amphotericin B.

In studies of the mechanism of action, the minimum fungicidal concentration of clotrimazole caused

leakage of intracellular phosphorus compounds into the ambient medium with concomitant breakdown of

cellular nucleic acids and accelerated potassium efflux. Both these events began rapidly and extensively

after addition of the drug.

Clotrimazole appears to be well absorbed in humans following oral administration and is eliminated

mainly as inactive metabolites. Following topical and vaginal administration, however, clotrimazole

appears to be minimally absorbed.

Six hours after the application of radioactive clotrimazole 1% cream and 1% solution onto intact and

acutely inflamed skin, the concentration of clotrimazole varied from 100 mcg/cm , in the stratum

corneum to 0.5 to 1 mcg/cm in the stratum reticulare, and 0.1 mcg/cm in the subcutis.

No measurable amount of radioactivity (≤0.001 mcg/mL) was found in the serum within 48 hours after

application under occlusive dressing of 0.5 mL of the solution or 0.8 g of the cream.

Only 0.5% or less of the applied radioactivity was excreted in the urine.

Following intravaginal administration of 100 mg

C-clotrimazole vaginal tablets to nine adult females,

an average peak serum level, corresponding to only 0.03 µg equivalents/mL of clotrimazole, was

reached 1 to 2 days after application. After intravaginal administration of 5 g of 1%

C-clotrimazole

vaginal cream containing 50 mg active drug, to five subjects (one with candidal colpitis), serum levels

corresponding to approximately 0.01 µg equivalents/mL were reached between 8 and 24 hours after

application.

INDICATIONS AND USAGE

Prescription clotrimazole topical solution product is indicated for the topical treatment of candidiasis

due to Candida albicans and tinea versicolor due to Malassezia furfur.

This formulation is also available as a nonprescription product which is indicated for the topical

treatment of the following dermal infections: tinea pedis, tinea cruris, and tinea corporis due to

Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton fluoccosum, and Microsporum canis.

CONTRAINDICATIONS

Topical antifungal agents are contraindicated in those patients with a history of hypersensitivity to any

of the components of the preparation.

WARNINGS

Clotrimazole topical solution is not for ophthalmic use.

PRECAUTIONS

General

If irritation or sensitivity develops with the use of clotrimazole, treatment should be discontinued and

appropriate therapy instituted.

Information for Patients

This information is intended to aid in the safe and effective use of this medication. It is not a disclosure

of all possible adverse or intended effects.

The patient should be advised to:

1. Use the medication for the full treatment time even though the symptoms may have improved. Notify

the physician if there is no improvement after 4 weeks of treatment.

2. Inform the physician if the area of application shows signs of increased irritation (redness, itching,

burning, blistering, swelling, oozing) indicative of possible sensitization.

3. Avoid sources of infection or reinfection.

Laboratory Tests

If there is lack of response to clotrimazole, appropriate microbiological studies should be repeated to

confirm the diagnosis and rule out other pathogens before instituting another course of antimycotic

therapy.

Drug Interactions

Synergism or antagonism between clotrimazole and nystatin, or amphotericin B, or flucytosine against

strains of C. albicans has not been reported.

Carcinogenesis, Mutagenesis, and Impairment of Fertility

An 18-month oral dosing study with clotrimazole in rats has not revealed any carcinogenic effect.

In tests for mutagenesis, chromosomes of the spermatophores of Chinese hamsters which had been

exposed to clotrimazole were examined for structural changes during the metaphase.

Prior to testing, the hamsters had received five oral clotrimazole doses of 100 mg/kg body weight. The

results of this study showed that clotrimazole had no mutagenic effect.

Usage in Pregnancy

The disposition of

C-clotrimazole has been studied in humans and animals. Clotrimazole is very

poorly absorbed following dermal application or intravaginal administration to humans. (See

CLINICAL PHARMACOLOGY.)

In clinical trials, use of vaginally applied clotrimazole in pregnant women in their second and third

trimesters has not been associated with ill effects.

There are, however, no adequate and well-controlled studies in pregnant women during the first

trimester of pregnancy.

Studies in pregnant rats with intravaginal doses up to 100 mg/kg have revealed no evidence of harm to

the fetus due to clotrimazole.

High oral doses of clotrimazole in rats and mice ranging from 50 to 120 mg/kg resulted in

embryotoxicity (possibly secondary to maternal toxicity), impairment of mating, decreased litter size and

number of viable young and decreased pup survival to weaning. However, clotrimazole was not

teratogenic in mice, rabbits and rats at oral doses up to 200, 180 and 100 mg/kg, respectively. Oral

absorption in the rat amounts to approximately 90% of the administered dose.

Because animal reproduction studies are not always predictive of human response, this drug should be

used only if clearly indicated during the first trimester of pregnancy.

Nursing Mothers

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human

milk, caution should be exercised when clotrimazole is used by a nursing woman.

Pediatric Use

Safety and effectiveness in pediatric patients have been established for clotrimazole when used as

indicated and in the recommended dosage.

ADVERSE REACTIONS

The following adverse reactions have been reported in connection with the use of clotrimazole:

erythema, stinging, blistering, peeling, edema, pruritius, urticaria, burning, and general irritation of the

skin.

OVERDOSAGE

Acute overdosage with topical application of clotrimazole is unlikely and would not be expected to

lead to a life-threatening situation.

DOSAGE AND ADMINISTRATION

Gently massage sufficient clotrimazole topical solution USP, 1% into the affected and surrounding skin

areas twice a day, in the morning and evening.

Clinical improvement, with relief of pruritus, usually occurs within the first week of treatment with

clotrimazole topical solution USP, 1%. If the patient shows no clinical improvement after 4 weeks of

treatment with clotrimazole topical solution USP, 1%, the diagnosis should be reviewed.

HOW SUPPLIED

Clotrimazole topical solution USP, 1% is supplied in 30 mL plastic bottles (NDC 72641-001-30);

boxes of one.

Store between 2° to 30°C (36° to 86°F).

Mfd. for: Tasman Pharma Inc.,

Warminster, PA 18974.

Made in New Zealand

Revised: February, 2019 308736

PRINCIPAL DISPLAY PANEL - 30 mL Bottle Carton

NDC 72641-001-30

Clotrimazole

Topical Solution

USP, 1%

FOR EXTERNAL

USE ONLY.

NOT FOR

OPHTHALMIC USE.

Keep this and all

medications out of the

reach of children.

Rx only 30 mL

Tasman Pharma

Tasman Pharma Inc.

CLOTRIMAZOLE TOPICAL SOLUTION USP, 1%

clotrimazole topical solution usp, 1% solution

Product Information

Product T ype

HUMAN PRESCRIPTION DRUG

Ite m Code (Source )

NDC:726 41-0 0 1

Route of Administration

TOPICAL

Active Ingredient/Active Moiety

Ingredient Name

Basis of Strength

Stre ng th

Clo trima zo le (UNII: G0 7GZ9 7H6 5) (Clo trimazo le - UNII:G0 7GZ9 7H6 5)

Clo trima z o le

10 mg in 1 mL

Inactive Ingredients

Ingredient Name

Stre ng th

po lyethylene g lyco l 4 0 0 (UNII: B6 9 78 9 4SGQ)

Packag ing

#

Item Code

Package Description

Marketing Start Date

Marketing End Date

1

NDC:726 41-0 0 1-30

1 in 1 CARTON

0 7/25/20 19

1

30 mL in 1 BOTTLE; Type 0 : No t a Co mbinatio n Pro duct

Marketing Information

Marke ting Cate gory

Application Numbe r or Monograph Citation

Marke ting Start Date

Marke ting End Date

ANDA

ANDA21228 1

0 7/25/20 19

Labeler -

T asman Pharma Inc. (080860172)

Revised: 8/2019

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